NANOKRISTAL TEKNOLOJISI: ÇÖZÜNÜRLÜĞÜ DÜŞÜK İLAÇLARIN ORAL BIYOYARARLANIMIN ARTIRILMASI

Year 2022, , 62 - 70, 10.02.2022

Yağmur Pirinçci Tok , Sevgi Güngör Yıldız Özsoy

https://doi.org/10.26650/JARHS2021-808337

Abstract

Nanokristal teknolojisi partikül boyutu 1000 nanometre (nm)’nin altında, herhangi bir taşıyıcı sisteme ihtiyaç duymadan katı ilaç partikülerinin üretilmesini sağlar. Sudaki çözünürlüğü düşük ilaçların partiküllerinin boyutunun küçültülmesi ile, yüzey alanlarının artması ve difüzyon tabakasının kalınlığının azaltılması k çözünürlük hızının da artışına yol açar. Buna bağlı olarak, absorpsiyon bölgesinde artan konsantrasyon gradienti bağırsak lümeni ve kan arasındaki pasif difüzyon yoluyla permeasyonu ve emilimi teşvik etmektedir. Dolayısıyla Biyofarmasötik Sınıflandırma Sistemi (BCS) Sınıf II ve IV’e ait ilaç molekülleri için nanokristal teknolojisi yaklaşımını kullanarak biyoyararlanımlarını geliştirmek ve/veya arttırmak oldukça önemlidir. Nanometre boyutunda ilaç partikülü elde edebilmek için yukarıdan aşağıya (top-down) ve aşağıdan yukarıya (bottom-up) yöntemlerinden yararlanılmaktadır. İlaç endüstrisinde uygulama kolaylığı, tekrar edilebilirliği ve ölçeklendirilebilmesi nedeniyle bilyeli değirmende yaş öğütme (BWM) ve yüksek basınçlı homojenizasyon (HPH) olarak alt bölümlere ayrılan yukarıdan aşağıya yöntemleri tercih edilmektedir. Nanokristal teknolojisi ile ilaç endüstrisinde hâlihazırda tedavide onaylanmış olan ilaç moleküllerinin daha az yan etki, daha düşük dozlar ve daha hızlı etki başlangıcı sağlayarak yeni dozaj formlarının geliştirilmesi ve yeni ilaç moleküllerinin daha iyi bir biyoyararlanımla formüle edilebilmesi amaçlanmaktadır.

Keywords

Nanokristal teknolojisi, suda çözünür ilaçlar, oral yol, hazırlama yöntemleri

NANOCRYSTAL TECHNOLOGY: INCREASING ORAL BIOAVAILABILITY OF LOW-SOLUBLE DRUGS

Abstract

Nanocrystal technology enables the production of solid drug particles with a particle size below 1000 nm without the need for any carrier system. By reducing the size of the particles of drugs with low solubility in water, increasing the surface area and decreasing the thickness of the diffusion layer leads to an increase in k the solubility rate. Accordingly, the increasing concentration gradient in the absorption zone promotes permeation and absorption by passive diffusion between the intestinal lumen and blood. Therefore, it is very important to improve and / or increase their bioavailability by using the nanocrystal technology approach for drug molecules belonging to BCS Class II and IV. Top-down and bottom-up methods are used to obtain nanometer-sized drug particles. In the pharmaceutical industry, top-down methods, which are subdivided into wet milling (BWM) and high pressure homogenization (HPH), are preferred in the ball mill because of its ease of application, repeatability and scalability. With nanocrystal technology, it is aimed to create new dosage forms by providing less side effects, lower doses and faster onset of action of drug molecules that are already approved in the pharmaceutical industry. It is also aimed that new drug molecules can be formulated with better bioavailability.

Keywords

Nanocrystal technology, Water-soluble drugs, Oral route, Methods of preparation

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